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Discovery of quorum quenchers targeting the membrane-embedded sensor domain of the Staphylococcus aureus receptor histidine kinase, AgrC.


ABSTRACT: We combined mRNA display technology with lipid-nanodisc based selections and identified high-affinity ligands targeting the integral membrane sensor domain of the histidine kinase AgrC as potent inhibitors of Staphylococcus aureus quorum sensing-modulated virulence. Our study highlights the potential of this integrated approach for identifying functional modulators of integral membrane proteins.

SUBMITTER: Xie Q 

PROVIDER: S-EPMC7530097 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature

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Discovery of quorum quenchers targeting the membrane-embedded sensor domain of the <i>Staphylococcus aureus</i> receptor histidine kinase, AgrC.

Xie Qian Q   Wiedmann Mareike M MM   Zhao Aishan A   Pagan Ivelisse R IR   Novick Richard P RP   Suga Hiroaki H   Muir Tom W TW  

Chemical communications (Cambridge, England) 20200901 76


We combined mRNA display technology with lipid-nanodisc based selections and identified high-affinity ligands targeting the integral membrane sensor domain of the histidine kinase AgrC as potent inhibitors of Staphylococcus aureus quorum sensing-modulated virulence. Our study highlights the potential of this integrated approach for identifying functional modulators of integral membrane proteins. ...[more]

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